Apixaban tablets and preparation method thereof

A technology of apixaban tablets and polyvinylpyrrolidone, which is applied in the field of apixaban tablets and its preparation, can solve the problems of low bioavailability, influence of drug absorption, and low dissolution rate in vitro, and achieve increased drug Absorption, facilitate large-scale production, reduce the effect of production process

Active Publication Date: 2018-09-21
北京阳光诺和药物研究股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, because apixaban is insoluble in water, it has the disadvantages of slow dissolution ...

Method used

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  • Apixaban tablets and preparation method thereof
  • Apixaban tablets and preparation method thereof
  • Apixaban tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1, preparation Apixaban tablet

[0032] The present embodiment provides the prescription and preparation method for preparing 10000 Apixaban tablets (the specification is 2.5mg / tablet), as follows:

[0033] Prescription composition:

[0034]

[0035] The apixaban used is apixaban powder, and its particle size is controlled at D90<30um; the adopted lactose, microcrystalline cellulose and magnesium stearate are passed through 80-mesh sieves respectively for use.

[0036] The preparation method comprises the following steps:

[0037] 1) Apixaban, polyethylene glycol-12-hydroxystearate and polyvinylpyrrolidone K30 were weighed and dissolved in 2.5L ethanol, and ultrasonically assisted to dissolve to obtain a transparent solution; Spray drying removes ethanol in the transparent solution to obtain apixaban solid dispersion; the process parameters of spray drying include: air inlet temperature 120°C, air outlet temperature 80°C, air volume 0.6m 3 / min, atomiza...

Embodiment 2

[0041] Embodiment 2, preparation Apixaban tablet

[0042] The present embodiment provides the prescription and preparation method for preparing 10000 Apixaban tablets (the specification is 2.5mg / tablet), as follows:

[0043] Prescription composition:

[0044]

[0045] The preparation method is basically the same as in Example 1.

Embodiment 3

[0046] Embodiment 3, preparation Apixaban tablet

[0047] The present embodiment provides the prescription and preparation method for preparing 10000 Apixaban tablets (the specification is 2.5mg / tablet), as follows:

[0048] Prescription composition:

[0049]

[0050]

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Abstract

The invention discloses apixaban tablets and a preparation method thereof. The apixaban tablets are prepared from the following raw materials: 20-30 parts of apixaban, 20-60 parts of HS-15, 10-30 parts of PVP-K30, 500-550 parts of lactose, 280-320 parts of microcrystalline cellulose, 45-55 parts of polyvinylpolypyrrolidone (PVPP) and 20-40 parts of coating premix, wherein the mass ratio of the HS-15 to the PVP-K30 is equal to (4 to 1)-(1 to 3). The preparation method comprises the following steps: (1) dissolving the apixaban, the HS-15 and the PVP-K30 in ethanol to obtain a transparent solution; then, spray-drying to obtain a solid dispersion; (2) evenly mixing the solid dispersion with the lactose, the microcrystalline cellulose and the PVPP and directly tabletting to obtain plain tablets; (3) coating the plain tablets to obtain the apixaban tablets. The tablets can significantly improve the dissolution rate of the medicine, increase medicine absorption, and improve the bioavailability, so that the therapeutic effect of the medicine can be fully exerted.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an apixaban tablet and a preparation method thereof. Background technique [0002] Apixaban (Apixaban), chemical name: 4,5,6,7-tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo- 1-piperidinyl)phenyl]-1H-oxazolo[3,4-C]pyridine-3-carbonylamine, American Chemical Abstracts registration number CAS: 503612-47-3, the structural formula is as follows: [0003] [0004] Apixaban is an oral selective inhibitor of activated factor Xa, jointly developed by Pfizer and Bristol-Myers Squibb. Apixaban can prevent blood clots, but the adverse reaction of bleeding is lower than that of the old drug warfarin. It is used for the prevention of blood clots in patients who have undergone hip or knee replacement surgery. [0005] Similar to rivaroxaban, apixaban has two binding sites for factor Xa, the 4-methoxyphenyl part in the structure of apixaban binds to the S1 pocket of factor Xa, and the...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K47/14A61K47/32A61K47/38A61K31/4545A61P7/02
CPCA61K9/2027A61K9/2031A61K9/2095A61K9/2866A61K31/4545A61P7/02
Inventor 罗桓利虔刘宇晶郑柏松李惠谌宗永
Owner 北京阳光诺和药物研究股份有限公司
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